New cyclobutyl analogs of nucleosides. Part 2. Synthesis and antiviral evaluation of 2-amino-7-[3,3-bis (hydroxymethyl)cyclobut-1-yl]-3H,7H-pyrrolo-[2,3-d]pyrimidin-4-one and of cyclobutyl analogs of the pyrimidine nucleosides
摘要:
The synthesis and antiviral evaluation of a series of 3,3-dihydroxymethyl cyclobutane nucleoside analogs related to the natural anti-HIV nucleoside, oxetanocin A are reported. The different purine and pyrimidine nucleoside analogs described in this paper have been obtained from 1-amino-3,3-dibenzyloxymethylcyclobutane. The compounds were tested against HSV-1, HCMV and HIV-1 in cell cultures, but none of them exhibited activity against these viruses. These results suggest the crucial role of the position of both hydroxymethyl groups in oxetanocin A and oxetanocin G for antiviral activity.
A series of 3-, 4-, and 5-pyridyl-2(1H)-quinolone derivatives with H or HO or CH3O substituents in the 8-position were prepared and tested for positive inotropic activity. Several derivatives, especially 29, 9b, and 27 with a pyridyl ring in the 5-position, were ca. 2-10 times more potent on left guinea pig atria than sulmazole (ARL-115) and milrinone used as references. Some structure-activity relationships
New cyclobutyl analogs of nucleosides. Part 2. Synthesis and antiviral evaluation of 2-amino-7-[3,3-bis (hydroxymethyl)cyclobut-1-yl]-3H,7H-pyrrolo-[2,3-d]pyrimidin-4-one and of cyclobutyl analogs of the pyrimidine nucleosides
The synthesis and antiviral evaluation of a series of 3,3-dihydroxymethyl cyclobutane nucleoside analogs related to the natural anti-HIV nucleoside, oxetanocin A are reported. The different purine and pyrimidine nucleoside analogs described in this paper have been obtained from 1-amino-3,3-dibenzyloxymethylcyclobutane. The compounds were tested against HSV-1, HCMV and HIV-1 in cell cultures, but none of them exhibited activity against these viruses. These results suggest the crucial role of the position of both hydroxymethyl groups in oxetanocin A and oxetanocin G for antiviral activity.